Cabal

Overdose

症状 (When taking drugs at doses of 5 tablets or more): There may be signs of poisoning in the form of drowsiness, anxiety in children, increased hypersensitivity, urinary retention, dry mouth, signs of anticholinergic effects in the form of constipation

Treatment: You stop taking the medicine, clean your stomach, take activated carbon and consult your doctor immediately。

Contraindications

Hypersensitivity to cetirizine, other ingredients of the drug, hydroxyzine.

Incompatibilities

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Examination of drug interactions with cetirizine and psoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide and antipyrin showed no clinically significant adverse interactions detected。

When used at the same time as theophylline (400 mg/m2), cetirizine's hoclearance is reduced by 16% (theophylline's kinetics do not change)。

When used at the same time as ritonavir, the AUC of cetirizine increased by 40%, but the same value of ritonavir changed slightly (-11%)。

Uses with macrolides (azithromycin, erythromycin) and ketoconahole showed no ECG change。

No data were available on the interaction with alcohol when using the substance at the volume of use (at the central alcohol concentration of 0.5g/l)。 However, to avoid central nervous system depression, you should refrain from drinking alcohol during drug treatment。

A three-day "cleaning" period is recommended prior to the appointment of an allergy test。1-Histamine receptor blockers block the development of skin allergic reactions。

No drug interactions between cetirizine and other drugs were observed。

Based on the results of an ongoing study of cetirizine drug interactions → 400 mg/day of pseudoephedrine or theophylline interactions, no clinically significant interactions were established。

The combination of cetirizine with alcohol and other drugs that suppress the central nervous system can contribute to a further reduction in concentration and rate of reaction, but cetirizine does not increase the effect of alcohol (at its concentration in 0.5g/l blood). )。

It is not advisable to combine the drug with other drugs without consulting a doctor。 Co-administration with a bronchodilator containing theophylline as an active substance increases the frequency of side effects of the drug Zincet。 No data has been obtained yet on the interaction of cetirizine with alcohol。 Nevertheless, consumption of alcoholic beverages in the treatment of drugs is not recommended。

It is not advisable to combine drug cabals with other drugs without consulting a doctor。 Co-administration with a bronchodilator containing theophylline as an active substance increases the frequency of side effects of the drug Cabal。 No data has been obtained yet on the interaction of cetirizine with alcohol。 Nevertheless, the use of alcoholic beverages in the treatment of covers is not recommended。

Undesirable effects

This drug is usually well tolerated。 Indigestion, abdominal pain, flatulence: In some cases, there may be headaches, drowsiness, dizziness, agitation, dry mouth, gastrointestinal disorders。 As an exception, there may be signs of hypersensitivity to the drug (urticaria, edema, shortness of breath)。 In this case, treatment with the drug should be stopped immediately and urgently consulted with the doctor。 You should inform your doctor about all aspects (rare) effects。

Therapeutic indications

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Treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis (itch, sneeze, stuffy nose, rhinorrhea, tearing, conjunctival hyperemia, etc.),

hay fever (pollen disease),

Urticaria (urticaria),

With allergic skin diseases, itching and rashes, including atopic dermatitis。

It has been shown to adults and children over 6 months for relief:

-Nose and eye symptoms of perennial (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis: itching, sneezing, stuffy nose, rhinorrhea, tearing, conjunctival congestion,

-Female-specific symptoms。

Allegiate rhinitis and conjunctivitis (including year-round and seasonal), hay fever (pollen), idiopathic ur measles and other allergic skin diseases with itching and rash

Allegiate rhinitis and conjunctivitis (including year-round and seasonal), hay fever (pollen), idiopathic ur measles and other allergic skin diseases with itching and rash

Pharmacotherapeutic group

  • H1-Antihistamines

Pharmacodynamic properties

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Cetirizine-active substance of drug cover® -It is a metabolite of hydroxyzine and belongs to the competitive histamine antagonist and block H group1-Histamine receptor

Cetirizine prevents onset, promotes the course of allergic reactions, and has pruritic and anti-ud effects. Cetirizine affects the early histamine-dependent stages of allergic reactions, limiting the release of inflammatory mediators later in allergic reactions, reducing eosinophils, neutrophils and basophils, and obese. Stabilize the membrane of cells。. Reduces capillary permeability, prevents the development of tissue edema, and relieves spasm in smooth muscle. Eliminate skin reactions to the introduction of histamine, certain allergens, and cooling (with cold urticaria)). Reduces histamine-induced bronchoconstriction in mild bronchial asthma

Cetirizine has no anticholinergic and anticerotonin effects。 At therapeutic doses, the drug does not substantially cause a sedative effect。 After a single dose of 10 mg cetirizine, the effect is expressed after 20 minutes (50% of patients) and after 60 minutes (95% of patients) and lasts more than 24 hours。Of course, against the background of treatment, cetirizine's resistance to antihistamine action does not develop。 After discontinuation of treatment, the effect lasts up to 3 days。

Cetirizine is a metabolite of hydroxyzine and belongs to the group of competing histamine antagonists and block H1-Histamine receptor

In addition to antihistamine, cetirizine prevents onset and facilitates the course of allergic reactions: late stage of eos bulb aggregation in skin and conjunctiva in patients exposed to atopies at 10 mg1 or 2 doses. To inhibit。

Clinical efficacy and safety。 A study of healthy volunteers found that the introduction of histamine in the skin at high doses of cetirizine at doses of 5 or 10 mg was significantly prohibited from rashes and redness, but no correlation with efficacy was established. Was shown.。 A 6-week placebo-controlled study with allergic rhinitis and concomitant bronchial asthma with mild and moderate severity found that taking cetirizine at a dose of 10 mg once daily reduces the symptoms of rhinitis and It was shown to have no effect on function。

The results of this study confirm the safety of cetirizine use in patients with allergies and mild to moderate bronchial asthma。

A placebo-controlled study showed that taking cetirizine at a dose of 60 mg/day for 7 days did not cause a clinically significant prolongation of the QT interval。 Taking cetirizine at the recommended dose improved the quality of life for patients with year-round and seasonal allergic rhinitis。

children。 A 5-12-day study involving a 35-year-old patient showed no signs of immunity to cetirizine's antihistamine effect。 Normal skin reactions to histamine recovered within 3 days of discontinuation of the drug due to its repeated use。

A 7-day placebo-controlled trial of cetirizine in a dosing-form syrup demonstrated drug safety in 6-11 months of patients aged 42 years。

Cetirizine was given twice with a dose of 0.25 mg/kg, which corresponded to approximately 4.5 mg/day (dose range was 3.4 to 6.2 mg/day)。

Pediatric use from 6 months to 12 months is only possible under the doctor's prescription and strict medical supervision。

Pharmacokinetic properties

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The pharmacokinetic parameters of cetirizine change linearly。

Suction。 After oral administration, the drug is rapidly and completely absorbed from the gastrointestinal tract。 Food intake does not affect the integrity of absorption, but its rate decreases。 In the development of organisms after a single return at the usage of CMax Concentration is 300ng/ml and reaches after (1±0.5) hours。

distribution。 Cetirizine binds (93 ± 0.3)% to plasma proteins。 Vd It's 0.5l/kg。 If the substance is used for 10 mg for 10 periods, cetirizine accumulation is not allowed。

Metabolism In quantity, it pushes in the body by O-dealkylation (say another h opponent1-Histamine receptor, metabolized in the liver by the cytochrome system) forms a pharmacologically inactive metabolite.

output。 In Osaka, T1/2 It's about 10 hours, 6 hours for children from 6 to 12 years, 5 hours for children from 2 to 6 years, 3.1 hours from 6 months to 2 years。 About 2/3 of the drug dose is excreted by the kidneys in an unchanged form。

In elderly patients and patients with chronic liver disease, a single dose of drug at a dose of 10 mg T is present1/2 It increases by about 50% and system clearance decreases by 40%。

In patients with mild renal failure (creatinine Cl> 40 ml/min), the pharmacokinetic parameters are similar to those in patients with normal renal function。

Patients with moderate renal failure and hemodialysis patients (creatinine Cl <7 ml/min) Teaching 10 mg T orally taking the drug1/2 It has been extended three times, reducing total clearance by 70% for these indicators in patients with normal renal function and requiring corresponding changes in the dosing regimen。

Cetirizine is not actually removed from the body during hemodialysis。

The bio-kinetic parameters of cetirizine when used in 5-60 mg usage change linearly。

Suction。 CMax In concentration, press after (1 ± 0.5) h and it is 300ng/ml。

Various biookinetic parameters such as CMax Plasma and AUC have good quality characteristics。

Food intake does not affect the complete absorption of cetirizine, but its rate decreases。 The bioavailability of various dosage forms of cetirizine (solutions, capsules, tablets) is comparable。

distribution。 Cetirizine binds (93 ± 0.3)% to plasma proteins。

Vd It's 0.5l/kg。 Cetirizine does not affect the binding of warfarin to proteins。

Metabolism Cetirizine does not undergo extensive primary metabolism。

output。 T1/2 It's about 10 hours。

No cetirizine accumulation was observed when the drug was taken at a daily dose of 10 mg for 10 days。

About 2/3 of the dose taken of the drug is excreted in the urine in an unchanged form。

Elderly patients。 In high school students who have a single recovery of microorganisms at a usage of 16 mg T, 101/2 It was higher than 50% and less organized than 40% compared to non-elderly patients。 Decreased cetirizine clearance in elderly patients is probably associated with reduced renal function in patients in this category。

Renal failure。 In patients with mild renal failure (creatinine Cl> 40 ml/min), the pharmacokinetic parameters are similar to those of healthy volunteers with normal renal function。

Patients with moderate renal failure and hemodialysis patients (creatinine Cl <7 ml/min) Teaching 10 mg T orally taking the drug1/2 It is extended three times and total clearance is reduced by 70% for healthy volunteers with normal renal function。

For patients with moderate or severe renal failure, corresponding changes in the dosing regimen are required (see "Dosing Method and Dose")。

Cetirizine is difficult to remove from the body during hemodialysis。

Liver failure Single dose of drug at a dose of 10 or 20 mg T in patients with chronic liver disease (hepatocyte, cholestasis and bile cirrhosis)1/2 It increases by about 50% compared to healthy people and reduces clearance by 40%。 Dose adjustments are only necessary for patients with liver failure and also associated renal failure。

children。 T1/2 For children from 6 to 12 years, it is reduced to 6 hours, 5 hours from 2 to 6 years, and 3.1 hours from 6 months to 2 years。

Name of the medicinal product

Cabal

Qualitative and quantitative composition

Cetirizine hydrochloride

Dosage (Posology) and method of administration

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中だ

Children and adults over 6 years old: Usage is 5 mg (1/2 table)。 Or October) Once, if you want, you can eat it at 10 mg (1 table。 Or 20 drops) once a day。 Sometimes the usage is 5 mg (1/2 table)。 Or 10 drops) can be sufficient to achieve therapeutic effect。 Usage is 10 mg (1 table。 Or 20 drops)。

Children from 6 months to 12 months: 2.5 mg (5 drops) 1 day。

Children from 1 to 2 years: Two times until 2.5 mg (5 drops)。

Children from 2 to 6 years: 2.5 mg (5 μ) 2 times or 5 mg (10 μ) 1 dose。

In the inex, the usage decreases according to the creatinine clearance: 30-49 ml/min—once in 5 mg creatinine kul, 10-29 ml/min—5 mg。

Since Cabal® It is excreted from the body by the kidneys and when prescribing drugs to patients with renal failure and elderly patients, the concentration of serum creatinine that can be calculated based on creatinine men who adjust the dose according to the amount of creatinine clearance, According to the formula:

Creatinine clearance, ml/min

Female creatinine clearance can be calculated by multiplying the obtained value by a factor of 0.85。

Renal failure Creatinine clearance, ml/min Medication regimen
Missing (norm) ≥80 10 mg/m2
Easy 50–79 10 mg/m2
平均 30–49 5 mg/m2
重い 10–29 5 mg every other time
End-stage-Patients undergoing hemodialysis <10 Taking medicine is contraindicated

In adult patients with renal and hepatic failure, the dose is according to the table above。

In children with renal failure, adjust the dose to account for creatinine clearance and body weight。

Patients with impaired liver function alone do not need to adjust their medication plans。

inside.

Drops are dissolved in a small amount of water before taking them。

Adults and adolescents over the age of 12: Once, preferably 10 mg (20 or 1) in the period。

Children from 6 to 12 years old: 5 mg (10 drops or 1/2 tablets) 2 times a day (morning and evening) or 10 mg (20 drops or 1 whole tablet) in the evening。

1-6 year old child Please shake the cover® A dosage form for oral administration。

Children from 2 to 6 years old: 5 mg (10 drops per day) once。 You can also divide this usage into two 2.5 mg (5 mg for both)。

Children 1-2 years: 2.5 mg (5l) 2 drinks。

Special patient group

You may need to reduce the patient's dose Elderly patients.

by Renal dysfunction Doses should be set individually depending on the function of the kidney。 The table below will help you select a dose。 To use this table, the subject's creatinine cl must be filled with ml/min。 After determining the creatinine concentration (mg/dl), the creatinine cl value can be determined using the formula:

Creatinine cl=[(140-circle, circle)×weight, kg)/(72-circle creatinine, mg/dl]

When calculating female creatinine clearance, the result should be multiplied by 0.85。 The table shows the usage according to cl of creatinine。

table

Dose selection by creatinine clearance

Creatinine clearance, ml/min 適量
≥80 10 mg time per day
50–79 10 mg time per day
30–49 5 mg time per day
11–29 5 mg twice a day
No. 10 (hemodialysis) 禁忌

insideDripping into a spoon or dissolving in water。

The amount of water that dissolves the drug should correspond to the amount of liquid that the patient (especially the child) can swallow。 The solution should be taken immediately after preparation。

Adult 10 mg (20 drops) once a day。 A 5 mg (10 mg) dose may be sufficient if a ring control for rice is possible。

Old times。 Elderly patients with normal renal function do not need to reduce the dose。

Renal dysfunction。 When prescribing a drug to a patient with renal impairment when alternative treatments cannot be prescribed, cetirizine is excreted mainly from the body by the kidneys, so the dose should be adjusted according to the amount of Cl creatinine。

The male Cl creatinine index can be calculated based on the concentration of serum creatinine in plasma using the formula:

Creatinine cl, ml/min = (140 x, loaf) x body weight, kg) / (72 x creatinine clShivalam, Mg/dl)。

Durable creatinine cl can be calculated by seeking a factor of 0.85 for the value obtained。

Renal failure Creatinine clearance, ml/min Medication regimen
Norm ≥80 10 mg/m2
Easy 50–79 10 mg/m2
平均 30–49 5 mg/m2
重い <30 5 mg every other time
End-stage-Patients undergoing hemodialysis <10 Taking medicine is contraindicated

Liver dysfunction。 Patients with liver dysfunction do not need to adjust their dosing regimens。 Dosage adjustments are recommended for patients with impaired liver and kidney function (see table above)。

children。 Pediatric use from 6 months to 12 months is only possible under the doctor's prescription and strict medical supervision。 6-12 months child-2.5 mg (5 drops) 1 time, 1 to 6 years-2.5 mg (5 drops) 2 times, 6-12 years-5 mg (10 drops) 2 times, 12 years or more-10 mg (20 drops) Once, sometimes an initial dose of 5 mg (10 drops) may be sufficient。

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Instructions for opening the bottle

The bottle closes with a safety device that prevents the child from opening it。 The bottle opens at a strong downward pressure on the lid, followed by an anti-clockwise twist。 After use, the bin crown must be tight and screwed。

inside, Swallow the whole with a little water, regardless of meal time。

The word Zincet is used as my prescription (to ask for a pass)。

2-6 year old child: 2.5 mg (1/2 teaspoon syrup) 2 days or 5 mg (1 teaspoon) 1 day, 6-12 year old child: 10 mg (1 table。 Or 2 teaspoons of syrup) 1 day or 5 mg (1/2 table。 Or 1 teaspoon of syrup) 2 wraps, wrap and wrapping, large parcel and 12 or more children: 10 mg (1 table。 Or 2 teaspoons of syrup) 1 day。

In the elderly or in patients with severe liver and/or renal damage, the drug is prescribed individually by the doctor, reducing the dose。

If you miss the time to take the drug by mistake, you should take the next dose as soon as possible。 If the next dose of the drug is approaching, the next dose should be taken according to the schedule without increasing the total dose。

inside, Swallow the whole with a little water, regardless of meal time。

Cabal is used as my disposal (to ask for a pass)。

2-6 year old child: 2.5 mg (1/2 teaspoon syrup) 2 days or 5 mg (1 teaspoon) 1 day, 6-12 year old child: 10 mg (1 table。 Or 2 teaspoons of syrup) 1 day or 5 mg (1/2 table。 Or 1 teaspoon of syrup) 2 wraps, wrap and wrapping, large parcel and 12 or more children: 10 mg (1 table。 Or 2 teaspoons of syrup) 1 day。

In the elderly or in patients with severe liver and/or renal damage, the drug is prescribed individually by the doctor, reducing the dose。

If you miss the time to take the drug by mistake, you should take the next dose as soon as possible。 If the next dose of the drug is approaching, the next dose should be taken according to the schedule without increasing the total dose。